期刊
JOURNAL OF CONTROLLED RELEASE
卷 91, 期 1-2, 页码 187-200出版社
ELSEVIER
DOI: 10.1016/S0168-3659(03)00232-3
关键词
pH-sensitive liposomes; acid-sensitive PEG conjugates; vinyl ether hydrolysis; acid-cleavable poly(ethylene glycol)-lipids
资金
- NIGMS NIH HHS [GM55266] Funding Source: Medline
Four structurally related, acid-labile polyethylene glycol (PEG) conjugated vinyl ether lipids have been synthesized and used at low molar ratios to stabilize the nonlamellar, highly fusogenic lipid, dioleoylphosphatidyl ethanolamine, as unilamellar liposomes. Acid-catalyzed hydrolysis of the vinyl ether bond destabilized these liposomes by removal of the sterically-stabilizing PEG layer, thereby promoting contents release on the hours timescale at pH<5. Structure-property correlations of these compounds suggested that single vinyl ether linkages between the PEG headgroup and the lipid backbone produce faster leakage rates. These studies also suggested that the presence of a slight negative charge at the membrane surface can accelerate the acid-catalyzed leakage process. (C) 2003 Elsevier B.V. All rights reserved.
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